Abstract: Disclosed is a method for replacing 7-lower alkylthio and 7-arylthio groups from cephalosporins with lower alkanoyloxy,lower alkoxy, aryloxy, aroyloxy, amino, lower alkylamino and azido moieties, and for replacing 6-lower alkylthio and 6-arylthio groups from penicillins with lower alkanoyloxy, lower alkoxy, aryloxy, aroyloxy, amino, lower alkyl amino, and azido moieties.

Abstract: 6-Amino and 6-benzalimino-6-arylthio penicillins are disclosed. These compounds are useful as intermediates in the preparation of 6-acylamino-6-arylthio penicillins.

Abstract: Compounds of the following general formula are useful in the treatment of sickle cell anemia: ##STR1## WHEREIN EACH OF R and R.sub.1 is hydrogen, chlorine, fluorine, bromine, trifluoromethyl, hydroxy, a lower alkoxy group of from 1 to 4 carbon atoms or a straight or branched lower alkyl group of from 1 to 4 carbon atoms; R.sub.2 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms; R.sub.3 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms, or when R.sub.2 is hydrogen, R.sub.3 is .beta.,.beta.,.beta.-trichloroethoxycarbonyl, benzyloxycarbonyl, p-methoxybenzyloxycarbonyl, p-nitrobenzyloxycarbonyl or tert-butoxycarbonyl; or NR.sub.2 R.sub.3 taken together form a monocyclic heterocyclic group selected from the group consisting of pyrrolidino, piperidino, morpholino, and N-(lower)alkylpiperazino; Z is ##STR2## wherein R.sub.4 is hydrogen or lower alkyl of from 1 to 4 carbon atoms, and R.sub.

Abstract: Thio-.beta.-lactam cephalosporins of the general formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, trihaloethyl, alkali metal or alkaline earth metal; R.sub.1 is hydrogen, lower alkyl, cycloalkyl, phenyl, phenoxy, phenyl-lower alkyl or certain heterocyclic groups; R.sub.2 is hydrogen, amino, carboxy, hydroxy or ureido; and X is hydrogen, hydroxy, lower alkylthio, lower alkylthiadiazolyl, lower alkyltetrazolyl or lower alkanoyloxy, are useful as antimicrobial agents.

Abstract: 6-Amino and 6-benzalimino-6-arylthio penicillins are disclosed. These compounds are useful as intermediates in the preparation of 6-acylamino-6-arylthio penicillins.

Abstract: New intermediates of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, trihaloethyl, alkali metal or alkaline earth metal and X is lower alkylthiadiazolylthio or lower alkyltetrazolylthio are useful for the production of antimicrobially active acyl derivatives thereof.

Abstract: Thio-.beta.-lactam cephalosporins of the general formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, trihaloethyl, alkali metal or alkaline earth metal; R.sub.1 is hydrogen, lower alkyl, cycloalkyl, phenyl, phenoxy, phenyl-lower alkyl or certain heterocyclic groups; R.sub.2 is hydrogen, amino, carboxy, hydroxy or ureido; and X is hydrogen, hydroxy, lower alkylthio, lower alkylthiadiazolyl, lower alkyltetrazolyl or lower alkanoyloxy, are useful as antimicrobial agents.

Abstract: Thio-.beta.-lactam cephalosporins of the general formula ##SPC1##Wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, trihaloethyl, alkali metal or alkaline earth metal; R.sub.1 is hydrogen, lower alkyl, cycloalkyl, phenyl, phenoxy, phenyl-lower alkyl or certain heterocyclic groups; R.sub.2 is hydrogen, amino, carboxy, hydroxy or ureido; and X is hydrogen, hydroxy, lower alkylthio, lower alkylthiadiazolyl, lower alkyltetrazolyl or lower alkanoyloxy, are useful as antimicrobial agents.

Abstract: Thio-.beta.-lactam penicillins of the general formula ##EQU1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, trihaloethyl, alkali metal or alkaline earth metal; R.sub.1 is hydrogen, lower alkyl, cycloalkyl, phenyl, lower alkoxyphenyl, phenoxy, phenyl-lower alkyl or certain heterocyclic groups; R.sub.2 is hydrogen, amino, carboxy or ureido; and n is 0 or 1; are useful as antimicrobial agents.

Abstract: Derivatives of difunctional compounds such as dicarboxylic acids, diisocyanates or diisothiocyanates wherein each functional group is reacted with 7-aminocephalosporanic acid or 7-aminodesacetoxycephalosporanic acid possess antibacterial activity.